1. Stem Cell/Wnt
    Anti-infection
    Autophagy
  2. Wnt
    β-catenin
    Bacterial
    Autophagy

Salinomycin (Synonyms: Procoxacin)

Cat. No.: HY-15597 Purity: >98.0%
Data Sheet SDS Handling Instructions

Salinomycin is an inhibitor of Wnt/β-catenin signaling, which acts on the Wnt/Fzd/LRP complex. Salinomycin strongly suppresses Wnt1-stimulated reporter activity with an IC50 of 163 nM, and reduces β-catenin levels.

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Salinomycin Chemical Structure

Salinomycin Chemical Structure

CAS No. : 53003-10-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO $99 In-stock
5 mg $70 In-stock
10 mg $120 In-stock
50 mg $390 In-stock
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Other Forms of Salinomycin:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Salinomycin is an inhibitor of Wnt/β-catenin signaling, which acts on the Wnt/Fzd/LRP complex. Salinomycin strongly suppresses Wnt1-stimulated reporter activity with an IC50 of 163 nM, and reduces β-catenin levels.

IC50 & Target

IC50: 163 nM (Wnt1-stimulated reporter)[1]

In Vitro

Salinomycin is a potent inhibitor of the Wnt signaling cascade. Incubation of the malignant lymphocytes with Salinomycin induces apoptosis within 48 h, with a mean IC50 of 230 nM. Salinomycin is also an antibiotic potassium ionophore, has been reported recently to act as a selective breast cancer stem cell inhibitor[1]. Salinomycin is a novel and an effective anticancer drug, inhibits SW620 cells and Cisp-resistant SW620 cells with IC50 of 1.54±0.23 μM and 0.32±0.05 μM, respectively. Salinomycin is found to have the ability to kill both cancer stem cells (CSCs) and therapy-resistant cancer cells. After continuous Salinomycin treatment for 48 h, the apoptotic cells are observed under the microscope and counted randomly at least 100 cells in one field. The number of apoptotic cells which are stained by Hoechst33342 is significantly increased in Cisp-resistant SW620 cells (20.20±3.72) than that of SW620 cells (9.40±2.07) per 100 cells (p<0.05). After treatment with Salinomycin for 48 h, flow cytometric analysis is used to detect the cell apoptosis both in SW620 cells and Cisp-resistant SW620 cells. The cell apoptotic rate in Cisp-resistant SW620 cells (37.82±3.63%) is significantly higher than that of SW620 cells (16.78±2.56%) (p<0.05)[2].

In Vivo

After administration of 4 mg/kg Salinomycin (Sal), 8 mg/kg Salinomycin and 10 uL/g saline water for 6 weeks, the mice are sacrificed. The size of the liver tumors in the Salinomycin treatment groups diminishes compare with the control group. The mean diameter of the tumors decreases from 12.17 mm to 3.67 mm (p<0.05) and the mean volume (V=length×width2×0.5) of the tumors decreases from 819 mm3 to 25.25 mm3 (p<0.05). Next, the tumors are harvested, followed by HE staining, immunohistochemistry, and TUNEL assays, to assess the anti-tumor activity of Salinomycin. HE staining shows that the structure of the liver cancer tissue:nuclei of different sizes, hepatic cord structure is destroyed. Immunohistochemistry shows that PCNA expression is lower after Salinomycin treatment. HE staining and TUNEL assays indicates the Salinomycin-treated groups has higher apoptosis rates than control. Furthermore, immunohistochemistry shows an increased Bax/Bcl-2 ratio after Salinomycin treatment. The protein expression of β-catenin decreases in the Salinomycin treatment groups compared with control[3]. Salinomycin is a kind of monocarboxylic acid polyether type antibiotics, produced by the fermentation of Streptomyces albus, possesses a specific cyclic structure, and can form a complex compound with the pathogenic microorganisms and the extracellular cations of coccidian, especially K+, Na+, Rb+, to alter the intracellular and extracellular ion concentrations[4].

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.3316 mL 6.6578 mL 13.3156 mL
5 mM 0.2663 mL 1.3316 mL 2.6631 mL
10 mM 0.1332 mL 0.6658 mL 1.3316 mL
Cell Assay
[2]

Salinomycin is dissolved in DMSO and stored, and then diluted with appropriate media before use[2].

For cisplatin or Salinomycin IC50 analysis in SW620 cells or Cisp-resistant SW620 cells, cells (1×104/well) are cultured in 96-well plates and treated with different chemotherapeutics (cisplatin, Salinomycin) in different concentrations for 48 h. Then 20 μL of cell counting kit-8 (CCK-8) is added into each of the 96-wells. After 4 h incubation at 37°C, the optical density (OD) values are detected at 450 nm using the scan reader. Cell growth inhibiting rates are described as cell inhibiting curves and the IC50 parameters (inhibiting concentration of 50% cells) are evaluated by Xlfit 5.2 software. For cell proliferation analysis, SW620 cells or Cisp-resistant SW620 cells (5×103/well) are also seeded in 96-well plates in serum-containing medium and treated with cisplatin (5 μM, according to the calculated IC50 values of cisplatin in SW620 cells) for 0, 12, 24, 48, 72 and 96 h. Then 20 μL cell counting kit-8 is added into each of the 96-wells. After 4-h incubation at 37°C, the coloring reactions are also quantified at 450 nm[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3][4]

Salinomycin is prepared in DMSO and then diluted with saline water (Mice and Rat)[3][4].

Mice[3]
Nude mice (nu/nu; 4-6 weeks of age) are used. HepG2 cells are suspended in 100 mL 1:1 serum-free DMEM and Matrigel. Mice are anesthetized with ketamine/xylazine and after surgically opening the abdomen, HepG2 cells are inoculated into the liver parenchyma and mice are monitored every 3 days for 35 days. Finally, 18 nude mice are divided into three groups that are intraperitoneally injected daily for 6 weeks: two Salinomycin-treated groups (4 mg/kg Salinomycin group, 8 mg/kg Salinomycin group) and the control group (saline water group).
Rat[4]
A total of 10 male rats are used in the experiment. After a routine anesthesia, the abdomen is opened. After a resuspension of high glucose medium not containing serum DMEM, and matrigel, the bladder transitional cancer cell line T24 is inoculated in the parenchyma of bladder in rats, and then the abdomen is sutured. After operation, the rats are randomized into the experiment group and the control group with five in each group. After operation, the rats in the experiment group are immediately given intraperitoneal injection of Salinomycin with a dosage of 8 mg/kg, while the rats in the control group are given intraperitoneal injection of normal saline. A close observation is paid during the drug administration period. After 15 d, the rats are sacrificed by cervical dislocation, and the complete tumor tissues are stripped to observe the tumor growth and metastasis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

751.0

Formula

C₄₂H₇₀O₁₁

CAS No.

53003-10-4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: >98.0%

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Product Name:
Salinomycin
Cat. No.:
HY-15597
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